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Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity |
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| Authors: | Butini Stefania Guarino Egeria Campiani Giuseppe Brindisi Margherita Coccone Salvatore Sanna Fiorini Isabella Novellino Ettore Belinskaya Tatyana Saxena Ashima Gemma Sandra |
| Institution: | European Research Centre for Drug Discovery and Development (NatSynDrugs), Via Aldo Moro 2, 53100 Siena, Italy. |
| Abstract: | Tacrine based reversible inhibitors of cholinesterases (ChEIs) containing peptidic tethers were synthesized to interact with specific regions at the gorge level, and their potency was determined with human (h) acetylcholinesterase and butyrylcholinesterase. Analogues 3i,j and 3l,m were identified as promising hits and may pave the way for the development of a new series of tacrine based enzyme selective hChEIs. |
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